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Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir.
Int J Pharm. 2016 Jan 30; 497(1-2):301-11.IJ

Abstract

The study investigated the influence of formulation parameters for design of self-microemulsifying drug delivery systems (SMEDDSs) comprising oil (medium chain triglycerides) (10%), surfactant (Labrasol(®), polysorbate 20, or Kolliphor(®) RH40), cosurfactant (Plurol(®) Oleique CC 497) (q.s. ad 100%), and cosolvent (glycerol or macrogol 400) (20% or 30%), and evaluate their potential as carriers for oral delivery of a poorly permeable antivirotic aciclovir (acyclovir). The drug loading capacity of the prepared formulations ranged from 0.18-31.66 mg/ml. Among a total of 60 formulations, three formulations meet the limits for average droplet size (Z-ave) and polydispersity index (PdI) that have been set for SMEDDSs (Z-ave≤100nm, PdI<0.250) upon spontaneous dispersion in 0.1M HCl and phosphate buffer pH 7.2. SMEDDSs with the highest aciclovir loading capacity (24.06 mg/ml and 21.12 mg/ml) provided the in vitro drug release rates of 0.325 mg cm(-2)min(-1) and 0.323 mg cm(-2)min(-1), respectively, and significantly enhanced drug permeability in the parallel artificial membrane permeability assay (PAMPA), in comparison with the pure drug substance. The results revealed that development of SMEDDSs with enhanced drug loading capacity and oral delivery potential, required optimization of hydrophilic ingredients, in terms of size of hydrophilic moiety of the surfactant, surfactant-to-cosurfactant mass ratio (Km), and log P of the cosolvent.

Authors+Show Affiliations

Apoteka Janković, Miloša Bajića 13, 21000 Novi Sad, Serbia.University of Belgrade, Faculty of Pharmacy, Department of Pharmaceutical Technology and Cosmetology, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: ljiljanadjek@gmail.com.University of Belgrade, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Vojvode Stepe 450, 11221 Belgrade, Serbia.University of Belgrade, Faculty of Pharmacy, Department of Pharmaceutical Technology and Cosmetology, Vojvode Stepe 450, 11221 Belgrade, Serbia.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26611669

Citation

Janković, Jovana, et al. "Evaluation of Critical Formulation Parameters in Design and Differentiation of Self-microemulsifying Drug Delivery Systems (SMEDDSs) for Oral Delivery of Aciclovir." International Journal of Pharmaceutics, vol. 497, no. 1-2, 2016, pp. 301-11.
Janković J, Djekic L, Dobričić V, et al. Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir. Int J Pharm. 2016;497(1-2):301-11.
Janković, J., Djekic, L., Dobričić, V., & Primorac, M. (2016). Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir. International Journal of Pharmaceutics, 497(1-2), 301-11. https://doi.org/10.1016/j.ijpharm.2015.11.011
Janković J, et al. Evaluation of Critical Formulation Parameters in Design and Differentiation of Self-microemulsifying Drug Delivery Systems (SMEDDSs) for Oral Delivery of Aciclovir. Int J Pharm. 2016 Jan 30;497(1-2):301-11. PubMed PMID: 26611669.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir. AU - Janković,Jovana, AU - Djekic,Ljiljana, AU - Dobričić,Vladimir, AU - Primorac,Marija, Y1 - 2015/12/01/ PY - 2015/08/25/received PY - 2015/11/04/revised PY - 2015/11/06/accepted PY - 2015/11/28/entrez PY - 2015/11/28/pubmed PY - 2016/10/16/medline KW - Aciclovir KW - Acyclovir KW - In vitro drug release KW - Parallel artificial membrane permeability assay (PAMPA) KW - Self-dispersing drug delivery systems KW - Self-microemulsifying drug delivery systems (SMEDDS) SP - 301 EP - 11 JF - International journal of pharmaceutics JO - Int J Pharm VL - 497 IS - 1-2 N2 - The study investigated the influence of formulation parameters for design of self-microemulsifying drug delivery systems (SMEDDSs) comprising oil (medium chain triglycerides) (10%), surfactant (Labrasol(®), polysorbate 20, or Kolliphor(®) RH40), cosurfactant (Plurol(®) Oleique CC 497) (q.s. ad 100%), and cosolvent (glycerol or macrogol 400) (20% or 30%), and evaluate their potential as carriers for oral delivery of a poorly permeable antivirotic aciclovir (acyclovir). The drug loading capacity of the prepared formulations ranged from 0.18-31.66 mg/ml. Among a total of 60 formulations, three formulations meet the limits for average droplet size (Z-ave) and polydispersity index (PdI) that have been set for SMEDDSs (Z-ave≤100nm, PdI<0.250) upon spontaneous dispersion in 0.1M HCl and phosphate buffer pH 7.2. SMEDDSs with the highest aciclovir loading capacity (24.06 mg/ml and 21.12 mg/ml) provided the in vitro drug release rates of 0.325 mg cm(-2)min(-1) and 0.323 mg cm(-2)min(-1), respectively, and significantly enhanced drug permeability in the parallel artificial membrane permeability assay (PAMPA), in comparison with the pure drug substance. The results revealed that development of SMEDDSs with enhanced drug loading capacity and oral delivery potential, required optimization of hydrophilic ingredients, in terms of size of hydrophilic moiety of the surfactant, surfactant-to-cosurfactant mass ratio (Km), and log P of the cosolvent. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/26611669/Evaluation_of_critical_formulation_parameters_in_design_and_differentiation_of_self_microemulsifying_drug_delivery_systems__SMEDDSs__for_oral_delivery_of_aciclovir_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(15)30358-6 DB - PRIME DP - Unbound Medicine ER -